CARBOHYDRATE POLYMERS
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2022
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IF 10.723
Kepeng Hu,Erna Jia,Qimeng Zhang,Wei Zheng,Rongjiao Sun,Mengao Qian,Ying Tan,Wanle Hu
Injectable hydrogel is of interesting for wound healing due to it can be used as carriers of bioactive molecules for the reparation of tissues with minimal invasiveness. However, the integration of lipid-soluble substances into hydrogel network is difficult because of the polarity differences. Here, the tea tree oil (TTO) is encapsulated into the hydrogel network via a previous emulsification process, and a tough and antibacterial injectable hydrogel is synthesized by the Schiff base reaction between carboxymethyl chitosan (CMCS) and genipin (GP). CMCS is served as both an emulsifier and a gel-forming material to construct the heterogeneous hydrogel. The obtained hydrogels present high adhesive strength (∼162.75 kPa), great antibacterial properties (over 90 %) and excellent biocompatibility. Moreover, an anal fistula-like wound healing experiment concluded that the heterogeneous hydrogel has good slow-release properties of TTO for an accelerate healing process, this hydrogel shows great potential for the treatment of complex anal fistula wounds.
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DOI
PubMed
高影响因子
PHYTOMEDICINE
·
2025
·
IF 8.3
Meichen Li,Yi Peng,Qingqing Xiao,Siyi Chen,Chunjie Zhang,Hongyu Chen,Yue Zhao,Shan Chang,Lu Qiu,Lele Zhang,Xiaoqiang Guo,Qiang Fu
Background Osteoarthritis (OA) is a chronic degenerative joint disease characterized by the degeneration of articular cartilage and synovial inflammation. Due to the ambiguity of its therapeutic targets, there are currently no effective interventions targeting the core mechanisms. Genipin is one of the main active components of the fruits of Gardenia jasminoides Ellis and shows great application potential in anti-inflammation and cartilage protection. Purpose This study aims to elucidate the direct molecular targets and underlying mechanisms of genipin in mitigating cartilage damage associated with osteoarthritis. Methods The in vitro curative effect of genipin was evaluated in the TNF- α -induced C28/I2 cell model. Potential therapeutic targets of genipin in OA was identified using CC-ABPP, SPR and other experiments. The binding sites of genipin were investigated by LC-MS/MS, molecular docking analysis and other methods. The therapeutic mechanism of genipin was further elucidated through the detection of changes in downstream metabolites and proteins. Results PGK1 has been identified as a key therapeutic target of genipin in OA. Genipin covalently binds to lysine 216 of PGK1, occupying its nucleotide-binding domain (NBD) domain and blocking ATP interaction, thereby competitively inhibiting PGK1 activity. Further studies revealed that genipin enhances methylglyoxal (MGO) levels, an upstream metabolite of PGK1, activating the Keap1-Nrf2 antioxidant pathway while suppressing NF- κ B-mediated inflammation, downregulating matrix metalloproteinase (MMPs) expression, reducing extracellular matrix (ECM) degradation, and ultimately protecting cartilage. Conclusion Genipin is a covalent PGK1 inhibitor. Genipin exerts its anti-OA effects by specifically targeting the NBD domain of PGK1 and regulating the Keap1-Nrf2/NF- κ B signaling pathway.
研究领域:
药理学
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分子生物学
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风湿病学
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骨关节炎研究
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药物发现
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DOI
PubMed
高影响因子
CARBOHYDRATE POLYMERS
·
2018
·
IF 5.158
Ting Wu,Weiping Liao,Wei Wang,Jie Zhou,Weiguo Tan,Weibing Xiang,Jinglin Zhang,Lina Guo,Tao Chen,Dong Ma,Weiye Yu,Xiang Cai
Lung-targeted genipin-crosslinked deacetylated chitosan (GEN-CS)/isoniazid (INH)/rifampin (RMP) nanogel particles (NGPs) were prepared as a treatment for tuberculosis caused by multidrug-resistant Mycobacterium tuberculosis (MTB) to surmount the undesirable side effects and decrease the cytotoxicity of INH and RMP when being against MTB. The size, morphology, in vitro release property, long-term antibacterial performance, stability, in vitro cytotoxicity, in vivo toxicity, and in vivo release property of GEN-CS/INH/RMP NGPs inhalation powder were investigated. The results showed that the GEN-CS/INH/RMP NGPs inhalation powder exhibited extended antibacterial activity because of its long-term release of INH and RMP. A simplex GEN-CS/INH/RMP NGPs pulmonary dose led to the therapeutic drug concentration of 40%–60% in lung and other organs (＜5%) for 24 h. Furthermore, this GEN-CS/INH/RMP NGPs lyophilized inhalation powder displayed lung-targeted property and lower in vivo toxicity. These results suggested that this GEN-CS/INH/RMP NGPs inhalation powder would be a more useful dosage form than separate dose of INH or RMP for MTB.
研究领域:
药剂学
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结核病治疗
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生物材料
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DOI
PubMed
高影响因子
Arabian Journal of Chemistry
·
2024
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IF 5.3
Xiaoyu Zhang,Ruihu Zhang,Rui Li,Jiaxing Zhang,Yuefei Wang,Xin Chai,Yuefei Wang
Gardenia blue (GB), a natural active blue pigment, can be synthesized from iridoid glycosides and primary amino-containing compounds in vivo and in vitro . However, limited studies have reported GB synthetic intermediates, leading to unawareness of the formation mechanism of GB. Here, we reported that GB could be detected in rats′ feces, whose formation was simulated by in vitro reaction of amino acid-rich feces extract from rats and genipin (GP) metabolized from geniposide (GE) through β -glucosidase. Firstly, we proved that 14 amino acids (AAs) detected in rats′ feces containing primary amino groups can react with GP to produce GB. Then, taking histidine (His) as example, we characterized the key intermediates during the reaction process, including basic units genihistidine A (GH-A) and dimers. As an active basic unit, GH-A underwent covalent polymerization to form dimer, which then self-assembled into supramolecular spherical nanoparticles through multiple noncovalent interactions, including hydrogen bonds, π-π interactions, and van der Waals interactions. Our study revealed the formation mechanism of GB and provided insights into the bioavailable form of GE from traditional Chinese medicine in vivo .
研究领域:
化学
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生物化学
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药理学
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中医药
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DOI
高影响因子
BIOMATERIALS
·
2021
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IF 12.479
Yaqiong Wang,Jingjing Guo,Bingjie Li,Dong Li,Zhaowei Meng,Shao-Kai Sun
Surgical adhesives have partly replaced traditional sutures to seal and reattach tissues due to their superiorities in preventing liquids leakage and avoiding secondary damage in the surrounding wound area. Most of the existing adhesives are committed to promoting wound healing and functional recovery. A therapeutic adhesive that assists in clearing the residual tumors in the surgical area is undoubtedly meaningful to obtain a better clinical outcome. Herein, enlightened by commercial BioGlue (albumin/glutaraldehyde sealant), a biocompatible therapeutic albumin/genipin bioglue is designed for postoperative wound adhesion and tumor ablation. The albumin/genipin bioglue is formed by simple mixing of bovine serum albumin (BSA) and genipin (GP) under a 35 °C water bath for 24 h without further purification . The obtained dark-blue fluorescent adhesive exhibits a significant temperature increase accompanied by heating-induced curing once irradiated with an 808-nm laser . This unique characteristic allows BSA-GP a therapeutic adhesive for postoperative wound adhesion and photothermal elimination of residual tumors under laser irradiation. Moreover, its easy injectability and impressive photothermal efficacy also make it feasible for in situ tumor photothermal ablation. The ultrasimple synthetic strategy by mimicking BioGlue endows BSA-GP adhesive with large-scale production capacity and clinical transformation potential, which is a successful paradigm for reforming existing clinical products.
研究领域:
生物材料
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外科手术
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癌症治疗
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材料科学
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DOI
PubMed
高影响因子
FISH & SHELLFISH IMMUNOLOGY
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2026
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IF 4.2
Lingjun Xie,Chushun Yi,Zhentao Ma,Songlin Luo,Shunqiang Wei,Xuemin Wei,Yinghui Wang,Aiguo Huang
Genipin inhibits WSSV replication in gill, hepatopancreas and muscle tissues in shrimp. • Genipin inhibits the expression of VP19, VP24, VP26, and VP28 in Drosophila S2 cells. • WSSV infection reprograms host metabolism to support viral replication. • Genipin exerts a bidirectional, dose-dependent modulation of host metabolism in shrimp. • PC and PEPCK are potential antiviral targets of genipin. White spot syndrome virus (WSSV) is the most devastating pathogen in shrimp aquaculture, causing massive economic losses worldwide. Current control strategies are limited due to the lack of adaptive immunity in crustaceans. In this study, the antiviral mechanism of genipin, a natural compound with known anti-WSSV activity, was investigated using a dual proteomic approach in Pacific whiteleg shrimp ( Litopenaeus vannamei ). In vitro fluorescence analysis confirmed that genipin specifically suppressed the expression of WSSV structural proteins. Through a four-group design (control, WSSV-infected, genipin-treated, and genipin-treated infected), 715 “drug-reversed” proteins were identified, whose WSSV-induced dysregulation was significantly restored by genipin. Protein set enrichment analysis and over-representation analysis revealed that genipin globally suppresses ribosome biogenesis and central carbon metabolic pathways, including the TCA cycle--pathways critical for viral replication. A concentration-gradient experiment further revealed differential regulation: genipin dose-dependently down-regulated cytoskeletal and metabolic components while up-regulating stress-responsive and adhesion modules, forming a “core response network” (CRN). Integrative cross-dataset analysis pinpointed two metabolic gatekeepers, pyruvate carboxylase (PC) and phosphoenolpyruvate carboxykinase (PEPCK), which exhibited hallmark virus-induced up-regulation and genipin-mediated reversal. Both enzymes occupy central positions linking the CRN to core metabolic pathways, suggesting a signal-metabolic coupling mechanism. Collectively, these results establish genipin as an agent that dismantles WSSV's metabolic support system potentially through modulation of PC and PEPCK, providing a promising strategy for combating viral diseases in shrimp aquaculture.
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DOI
PubMed
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
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2016
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IF 3.42
Yan Zhang,Lina Mao,Juan Liu,Tianjun Liu
A kind of self-fluorescent, biocompatible, and low-toxic Genipin crosslinked Globin-PEI nanoparticle (Gb-G-PEI NP) with high enzymolysis-stability and photo-stability was synthesized successfully. The properties of the Gb-G-PEI NP were characterized, including its particle size, surface zeta potential, morphology, paclitaxel (PTX) loading capacity and release. The Gb-G-PEI NPs as imaging probe were investigated by Confocal Laser Scanning Microscope (CLSM) in vitro and by fluorescence imaging system in vivo . Cell imaging results showed that the tumor cell line (HepG-2) had the faster cell uptake rate and metabolism rate than the normal cell line (L-O2), this difference showed its tumor selectivity. MTT assay revealed that the PTX-loaded Gb-G-PEI NPs showed almost the equal potence to tumor cell HepG-2 as the free PTX at the same PTX concentration, while a lower cytotoxicity to normal cell L-O2, suggesting its promising utilization as a drug delivery system. The imaging on mice demonstrated the possibility of the self-fluorescent Gb-G-PEI NPs as probe in vivo . So Gb-G-PEI NPs can be potentially utilized as both tracking marker and tumor cell selective drug delivery system in the biomaterial field.
研究领域:
生物材料学
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药剂学
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分子生物学
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DOI
PubMed
高影响因子
LANGMUIR
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2025
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IF 3.9
Shi-Hao Yang,Xue Zhang,Yu-Mei Tan,Rui Xie,Wei Wang,Zhuang Liu,Da-Wei Pan,Xiao-Jie Ju,Liang-Yin Chu
The controllable fabrication and performances of monodisperse genipin-cross-linked gelatin–chitosan composite (GGC) embolic microspheres with both uniform sizes and adjustable characteristics of elasticity and degradation are reported for the first time. Monodisperse emulsion droplets are fabricated as templates by using gelatin and chitosan aqueous solution as the disperse phase in a microfluidic device, and the chemical cross-linking of gelatin and chitosan inside droplet templates is achieved with genipin that transfers from the collection bath into the droplets. The sizes of droplet templates and the resultant GGC microspheres can be flexibly controlled and predicted by adjusting the fluid flow rates and the device dimensions. The elastic property of GGC microspheres can be flexibly regulated by adjusting the molar ratio of gelatin/chitosan in the disperse phase. The in vitro degradation-caused dynamic volume shrinkage of GGC microspheres can be flexibly regulated by adjusting the molar ratio of gelatin/chitosan, the chitosan deacetylation degree, and the enzyme concentration in degradation solution. Based on the Box–Behnken design-response surface method, a second-order equation is developed for the first time to predict the in vitro degradation-caused dynamic volume shrinkage ratios of microspheres prepared with different molar ratios of gelatin/chitosan and different chitosan deacetylation degrees in degradation solutions with different enzyme concentrations. The fabricated GGC microspheres show good repeatable embolization performances in an in vitro embolization chip system. The results of this study provide valuable guidance for controllable fabrication of degradable microspheres with both uniform sizes and on-demand elastic and degradation characteristics for efficient application in embolization therapy.
研究领域:
生物材料学
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介入医学
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2025
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IF 8.5
Nanting Zhu,Decheng Bi,Jinfeng Huang,Lijun Yao,Yan Wu,Zedong Jiang,Zhangli Hu,Beiwei Zhu,Shuangfei Li,Xu Xu
In this study, genipin served as crosslinker to combine sodium caseinate (SC) and chitosan oligosaccharide (COS), aiming to improve the physicochemical properties and encapsulation efficiency of SC in delivering hydrophobic nutritional factors. The genipin crosslinked complex of SC and COS (GSCC) was characterized by circular dichroism spectrum and infrared spectrum analyses. Nanoparticles produced from GSCC (GSCCNP) exhibited a superior hydrophilicity compared to those derived from SC (SCNP). GSCCNP significantly augmented the encapsulation efficacy and photostability of β-carotene. β-Carotene encapsulated within GSCCNP (βC-GSCCNP) exhibited remarkable in vitro sustained release characteristics and heightened bioavailability. In addition, βC-GSCCNP showed significant in vitro anti-inflammatory activity. These findings indicated that genipin crosslinking COS-modified SC could construct a nano-delivery system to enhance the stability and bioavailability of insoluble nutritional factors, thereby presenting promising applications for hydrophobic nutrients in the development of functional foods and beverages.
研究领域:
食品科学
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营养学
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生物化学
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DOI
PubMed
高影响因子
Polymers
·
2024
·Vol. 16
·期 20
·2876
·
IF 4.7
Ling Wang,Xiaoyue Ding,Xiaorui He,Ning Tian,Peng Ding,Wei Guo,Oseweuba Valentine Okoro,Yanfang Sun,Guohua Jiang,Zhenzhong Liu,Armin Shavandi,Lei Nie
Multifunctional hydrogel dressings remain highly sought after for the promotion of skin wound regeneration. In the present study, multifunctional CHS-DA/HACC (CH) hydrogels with an interpenetrated network were constructed using hydroxypropyl trimethyl ammonium chloride modified chitosan (HACC) and dopamine-modified chondroitin sulfate (CHS-DA), using genipin as crosslinker. The synthesis of HACC and CHS-DA was effectively confirmed using Fourier transform infrared (FT-IR) analysis and1H nuclear magnetic resonance (1H NMR) spectroscopy. The prepared CH hydrogels exhibited a network of interconnected pores within the microstructure. Furthermore, rheological testing demonstrated that CH hydrogels exhibited strong mechanical properties, stability, and injectability. Further characterization investigations showed that the CH hydrogels showed favorable self-healing and self-adhesion properties. It was also shown that increasing HACC concentration ratio was positively correlated with the antibacterial activity of CH hydrogels, as evidenced by their resistance toEscherichia coliandStaphylococcus aureus. Additionally, Cell Counting Kit-8 (CCK-8) tests, fluorescent images, and a cell scratch assay demonstrated that CH hydrogels had good biocompatibility and cell migration ability. The multifunctional interpenetrated network hydrogels were shown to have good antibacterial properties, antioxidant properties, stable storage modulus and loss modulus, injectable properties, self-healing properties, and biocompatibility, highlighting their potential as wound dressings in wound healing applications.
研究领域:
生物材料学
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再生医学
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药剂学
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DOI
PubMed
高影响因子
Asian Journal of Pharmaceutical Sciences
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2018
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IF 4.56
Yibin Yu,Ruoxi Feng,Jinyu Li,Yuanyuan Wang,Yiming Song,Guoxin Tan,Dandan Liu,Wei Liu,Xinggang Yang,Hao Pan,Sanming Li
The objective of this study was to develop a novel hybrid genipin-crosslinked dual-sensitive hydrogel/nanostructured lipid carrier (NLC) drug delivery platform. An ophthalmic anti-inflammatory drug, baicalin (BN) was chosen as the model drug. BN NLC was prepared using melt-emulsification combined with ultra-sonication technique. Additionally, a dual pH- and thermo-sensitive hydrogel composed of carboxymethyl chitosan (CMCS) and poloxamer 407 (F127) was fabricated by a cross-linking reaction with a nontoxic crosslinker genipin (GP). GP-CMCS/F127 hydrogel was characterized by FTIR, NMR, XRD and SEM. The swelling studies showed GP-CMCS/F127 hydrogel was both pH- and thermo-sensitive. The results of in vitro release suggested BN NLC gel can prolong the release of baicalin comparing with BN eye drops and BN NLC. Ex vivo cornea permeation study was evaluated using Franz diffusion cells. The apparent permeability coefficient ( P app ) of BN NLC gel was much higher (4.46-fold) than that of BN eye drops. Through the determination of corneal hydration levels, BN NLC gel was confirmed that had no significant irritation to cornea. Ex vivo precorneal retention experiments were carried out by a flow-through approach. The results indicated that the NLC-based hydrogel can prolong precorneal residence time. In conclusion, the hybrid NLC-based hydrogel has a promising potential for application in ocular drug delivery.
研究领域:
药剂学
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生物材料学
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眼科药物研究
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2026
·
IF 8.5
Lei Nie,Xiaoyue Ding,Yiran Lin,Letian Yan,Yanting Han,Yuanna Sun,Yanfang Sun,Guohua Jiang
Decellularized extracellular matrix (dECM) has been widely used in tissue engineering and regenerative medicine due to its excellent biocompatibility and biological activities. In this work, the dECM was obtained by treating porcine Achilles tendon tissue via a combination of chemical, physical, and biological approaches. The obtained dECM was interpenetrated with genipin crosslinked quaternary ammonium chitosan (QCS) network to fabricate the composite genipin/QCS/dECM (QGD) hydrogels. The prepared QGD hydrogels exhibited an interconnected microstructure and a suitable water-absorption capacity. Furthermore, the QGD hydrogels exhibited strong adhesion to the surfaces of different matrices and various organs, including lung, liver, trachea, heart, and spleen. The remodelling of dECM gave the QGD hydrogels adjustable self-healing ability and mechanical properties. In addition, the QGD bio-adhesives exhibit effective antibacterial activity against the typical Gram-positive S. aureus and Gram-negative E. coli . 2,2′-Azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS) radical scavenging and 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging tests confirmed the antioxidant abilities of QGD hydrogels, and the cellular reactive oxygen species (ROS) scavenging potential was also investigated using RAW264.7 cells. Furthermore, the QGD hydrogels possessed excellent hemocompatibility, cytocompatibility, and cell pro-migration abilities. The results confirmed that the proposed QGD hydrogels could serve as potential bioadhesives for biomedical applications.
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高影响因子
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